Aminoglycoside胺基配糖體抗生素
抗藥性 例子 *注射 **capreomycin:second-line agent of tuberculosis,amikacin-resistant **spectinomycin(IM): no Cross-resistance with other aminoglycosides, alternative treatment for drug-resistant gonorrhea(淋病) or gonorrhea in penicillin-allergic patients. **streptomycin: , use as second-line agent for treatment of turberculosis **gentamicin: most , active to G(+) ***enterococcus resistant to it for their enzyme, thus we can use streptomycin to treat it. **sisomicin: similar to gentamicin **netilmicin:spectrum is the same to that of gentamicin and tobramycin, can treat gentamicin-resistant G(-) and tobramycin-resistant G(-). **tobramycin(半合成自kanamycin B): most , spectrum and PK are similar to gentamicin, 用於長期投與 **amikacin(半合成自kanamycin A): gentamicin-resistant G(-),tobramycin-resistant G(-), multidrug-resistant Mycobacterium tuberculosis including streptomycin-resistant one often susceptable to it. *口服 and 局部 **kanamycin: Pseudomonas and Streptococcus are resistant 抗生素的抗菌譜特色 **neomycin: . Pseudomonas and Streptococcus are resistant **paramomycin *gentamicin, kanamycin, and neomycin can treat G(+) *交叉抗藥性: **amikacin(半合成自kanamycin A)和kanamycin **kanamycin和neomycin 機轉 *抑制initiation(所以殺菌) *和elongation by binding to 30s(irreversible) 治療學 *aminoglycoside is widely against G(-), especially in bacteremia and sepsis **such as enteric bacteria **和Beta-lactam antibiotics一起使用可以增強對G(+)的效用 *because the process aminoglycosides across cell membrane into the cytoplasm is a oxygen-dependant secondary active transportation, it can be used to kill G(-) aerobes only, anaerobes are not susceptable . *the transmembrane electrochemical gradien supplies the energy for this process, and transport is coupled to a proton pump. *low extracellular pH and anaerobic condition inhibit transport by reducing gredient. *cell wall-active drug:penicillins, vancomycin, when used with Aminoglycosides, transport of aminoglycosides into cell is enhanced. *once daily dosing 是因為後抗生素效應 *in the infection of Streptococcal, Staphylococcal, and enterococcal Endocarditis, thrice-daily administration is still recommended. **和Beta-lactam antibiotics一起使用可以增強對G(+)的效用 **gentamicin is not active to Streptococcal, and enterococcal **when treat infection of Staphylococcal, Gentamicin often be used with vancomycin and penicillins. *some of the administered aminoglycosides can pass BBB only when active inflammation presents. **for higher conc. , intrathecal and intraventricular injection is needed. **however, this therapy has benn substituted by third generation cephalosporin. *cannot be used as single agent to treat pneumonia for poor penatration 配伍 *cell wall-active drug:penicillins, vancomycin, when used with Aminoglycosides, transport of aminoglycosides into cell is enhanced. *和Beta-lactam antibiotics一起使用可以增強對G(+)的效用 *Aminoglycoside are in combination with vancomycin or a penicillins for endocarditis, and for treatment of tuberculosis **gentamicin(aminoglycoside)+vancomycin is the alternative of enterococcal endocarditis *Streptomycin plus Penicillins is effective for **enterococcal endocarditis **virdans streptococcal endocarditis *third-generation cephalosporins **Empirical therapy of sepsis of unknown cause in both the immunocompetent and the immunocompromised patient. **in neutropenic, febrile immunocompromised patients, third-generation cephalosporins are often used in combination with an aminoglycosides. *Imipenem and Meropenem with or without Aminoglycoside can treat febrile neutropenic patients(發燒型嗜中性白血球低下症) *oral tetracyclines often coadministrate with Aminoglycoside to treat plague(鼠疫), tularenia(兔熱病), and brucellosis(布氏桿菌症) **1g/d (15mg/kg/d for children) streptomycin is given IM in combination with an oral tetracycline. 毒性 *腎毒性和耳毒性 **腎毒性:reversible **耳毒性:irreversible *if used in pregnancy, it may cause deafness in newborn. *toxicity is both concentration-dependent and time-dependent *if the trough conc.(波谷濃度) is above 2μg/ml , toxicity may happen. *toxicity is less possible to happen in Once daily dosing **if the therapy is longer than 2~3 days, serum conc. need be routinely checked, depends on renal function. *If streptomycin was used over 6 months in TB, the toxicity may happen *if used with loop diuretics may potentiate nephrotoxicity. *高劑量的時候可能會像curare一樣產生作用:give calcium gluconate (give promptly) or neostigmine 解毒 重點 *aminoglycoside is widely against G(-), especially in bacteremia and sepsis **such as enteric bacteria **和Beta-lactam antibiotics一起使用可以增強對G(+)的效用 *once daily dosing 是因為後抗生素效應 *in the infection of Streptococcal, Staphylococcal, and enterococcal Endocarditis, thrice-daily administration is still recommended. **和Beta-lactam antibiotics一起使用可以增強對G(+)的效用 **gentamicin is not active to Streptococcal, and enterococcal **when treat infection of Staphylococcal, Gentamicin often be used with vancomycin and penicillins. *gentamicin: most , active to G(+) **enterococcus resistant to it for their enzyme, thus we can use streptomycin to treat it. *口服 and 局部 **kanamycin: Pseudomonas and Streptococcus are resistant 抗生素的抗菌譜特色 **neomycin: . Pseudomonas and Streptococcus are resistant **paramomycin *Aminoglycoside are in combination with vancomycin or a penicillins for endocarditis, and for treatment of tuberculosis **gentamicin(aminoglycoside)+vancomycin is the alternative of enterococcal endocarditis *Streptomycin plus Penicillins is effective for **enterococcal endocarditis **virdans streptococcal endocarditis *third-generation cephalosporins **Empirical therapy of sepsis of unknown cause in both the immunocompetent and the immunocompromised patient. **in neutropenic, febrile immunocompromised patients, third-generation cephalosporins are often used in combination with an aminoglycosides. *Imipenem and Meropenem with or without Aminoglycoside can treat febrile neutropenic patients(發燒型嗜中性白血球低下症) 參考資料 basic2007 Category:配醣體 Category:抗生素:抑制蛋白質生合成 Category:腎毒性 Category:有耳毒性的藥物 分類:抗格蘭氏陰性菌 分類:IV 分類:oral 分類:IM 分類:concentration-dependent 分類:kill 分類:局部 分類:腎臟排泄 分類:廣效型抗生素